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European Journal of Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/29332198/drug-delivery-and-transport-into-the-central-circulation-an-example-of-zero-order-in-vivo-absorption-of-rotigotine-from-a-transdermal-patch-formulation
#1
Willi Cawello, Marina Braun, Jens-Otto Andreas
BACKGROUND AND OBJECTIVE: Pharmacokinetic studies using deconvolution methods and non-compartmental analysis to model clinical absorption of drugs are not well represented in the literature. The purpose of this research was (1) to define the system of equations for description of rotigotine (a dopamine receptor agonist delivered via a transdermal patch) absorption based on a pharmacokinetic model and (2) to describe the kinetics of rotigotine disposition after single and multiple dosing...
January 13, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29305813/a-simultaneous-mixed-effects-pharmacokinetic-model-for-nefopam-n-desmethylnefopam-and-nefopam-n-oxide-in-human-plasma-and-urine
#2
Aravind Mittur
BACKGROUND AND OBJECTIVE: Nefopam is a non-opioid, non-steroidal, central analgesic thought to act via multiple mechanisms including potent inhibition of serotonin-norepinephrine reuptake and modulation of voltage-sensitive calcium and sodium channels. There has been a resurgence in its use for postoperative pain and neuropathic pain. Dosing route-dependent metabolism and clinical effects have been described following intravenous and oral nefopam. N-desmethylnefopam and nefopam N-oxide are metabolites of clinical interest...
January 5, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29264831/cyp-suppression-in-human-hepatocytes-by-monomethyl-auristatin-e-the-payload-in-brentuximab-vedotin-adcetris%C3%A2-is-associated-with-microtubule-disruption
#3
Francis S Wolenski, Cindy Q Xia, Bingli Ma, Tae H Han, Wen C Shyu, Suresh K Balani
BACKGROUND AND OBJECTIVES: Monomethyl auristatin E (MMAE), the toxin linked to CD30-specific monoclonal antibody of Adcetris® (brentuximab vedotin), is a potent anti-microtubule agent. Brentuximab vedotin has been approved for the treatment of relapsed or refractory Hodgkin lymphoma and anaplastic large cell lymphoma. Cytochrome P450 (CYP) induction assessment of MMAE was conducted in human hepatocytes to assess DDI potentials and its translation to clinic. METHODS: MMAE was incubated at 1-1000 nM with cultured primary human hepatocytes for 72 h, and CYP1A2, CYP2B6, and CYP3A4 mRNA expression was assessed by quantitative reverse transcription-polymerase chain reaction and CYP-specific probe substrate by liquid chromatography coupled with mass spectrometry, along with microtubule disruption by immunofluorescence staining using anti-β-tubulin antibody and imaging...
December 20, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29260505/vancomycin-dosing-and-monitoring-critical-evaluation-of-the-current-practice
#4
Fawzy Elbarbry
After more than six decades of its use as the mainstay antibiotic for the treatment of multidrug-resistant Gram-positive bacterial infections, dosing and monitoring of vancomycin therapy have not been optimized. The current vancomycin therapeutic guidelines recommend empiric doses of 15-20 mg/kg administered by intermittent infusion every 8-12 h in patients with normal kidney function. Additionally, the guidelines recommend trough concentration of 15-20 mg/L as a therapeutic goal for adult patients with severe infections...
December 19, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29250739/prediction-of-tumor-to-plasma-ratios-of-basic-compounds-in-subcutaneous-xenograft-mouse-models
#5
Prashant B Nigade, Jayasagar Gundu, K Sreedhara Pai, Kumar V S Nemmani
BACKGROUND: Predicting target site drug concentrations is of key importance for rank ordering compounds before proceeding to chronic pharmacodynamic models. We propose generic tumor-specific correlation-based regression equations to predict tumor-to-plasma ratios (tumor-Kps) in slow- and fast-growing xenograft mouse models. METHODS: Disposition of 14 basic small molecules was investigated extensively in mouse plasma, tissues and tumors after a single oral dose administration...
December 18, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29247332/pharmacokinetics-safety-and-tolerability-of-single-dose-elbasvir-in-participants-with-hepatic-impairment
#6
William L Marshall, Hwa-Ping Feng, Larissa Wenning, Graigory Garrett, Xiaobi Huang, Fang Liu, Deborah Panebianco, Luzelena Caro, Christine Fandozzi, Kenneth C Lasseter, Richard A Preston, Thomas Marbury, Joan R Butterton, Marian Iwamoto, Wendy W Yeh
BACKGROUND: The combination of elbasvir and grazoprevir is approved for the treatment of hepatitis C virus genotype 1 or 4 infection. OBJECTIVE: To evaluate the pharmacokinetics and safety of single-dose elbasvir 50 mg in participants with hepatic impairment. METHODS: Participants with mild, moderate, or severe hepatic impairment and age-, sex-, and weight-matched healthy controls were enrolled in a 3-part, open-label, sequential-panel, single-dose pharmacokinetic study...
December 15, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29236211/association-of-whole-blood-tacrolimus-concentrations-with-kidney-injury-in-heart-transplantation-patients
#7
Maaike A Sikma, Claudine C Hunault, Johannes H Kirkels, Marianne C Verhaar, Jozef Kesecioglu, Dylan W de Lange
BACKGROUND AND OBJECTIVES: Acute kidney injury (AKI) is frequently observed after heart transplantation and is associated with morbidity and mortality. However, many confounding factors also contribute to the development of AKI in heart transplants. We hypothesized that supratherapeutic whole-blood tacrolimus trough concentrations are associated with AKI. METHODS: In a retrospective observational cohort from April 2005 to December 2012, all adult heart transplantation patients were included...
December 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29204788/modeling-drug-disposition-and-drug-drug-interactions-through-hypothesis-driven-physiologically-based-pharmacokinetics-a-reversal-translation-perspective
#8
LETTER
Guo-Fu Li, Qing-Shan Zheng
No abstract text is available yet for this article.
December 5, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29164523/identification-of-uridine-5-diphosphate-glucuronosyltransferases-responsible-for-the-glucuronidation-of-mirabegron-a-potent-and-selective-%C3%AE-3-adrenoceptor-agonist-in-human-liver-microsomes
#9
Kentaro Konishi, Daisuke Tenmizu, Shin Takusagawa
BACKGROUND AND OBJECTIVES: Mirabegron is cleared by multiple mechanisms, including drug-metabolizing enzymes. One of the most important clearance pathways is direct glucuronidation. In humans, M11 (O-glucuronide), M13 (carbamoyl-glucuronide), and M14 (N-glucuronide) have been identified, of which M11 is one of the major metabolites in human plasma. The objective of this study was to identify the uridine 5'-diphosphate (UDP)-glucuronosyltransferase (UGT) isoform responsible for the direct glucuronidation of mirabegron using human liver microsomes (HLMs) and recombinant human UGTs (rhUGTs)...
November 21, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29134502/the-influence-of-compatibility-of-rhubarb-and-radix-scutellariae-on-the-pharmacokinetics-of-anthraquinones-and-flavonoids-in-rat-plasma
#10
Yaqing Zhang, Zunjian Zhang, Rui Song
BACKGROUND AND OBJECTIVES: Rhubarb-Radix scutellariae is a classic herb pair, which is commonly used to clear away heat and toxin in clinic. The aim of this study was to investigate the influence of compatibility of Rhubarb and Radix scutellariae on the pharmacokinetic behaviors of anthraquinones and flavonoids in rat plasma. METHODS: Eighteen rats were randomly divided into three groups, and were orally administered Rhubarb and/or Radix scutellariae extracts. A sensitive and rapid UPLC-MS/MS method was developed and validated to determine the concentrations of baicalin, baicalein, wogonside, wogonin, rhein, and emodin in rat plasma...
November 14, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29134501/pharmacokinetic-properties-of-saffron-and-its-active-components
#11
Azar Hosseini, Bibi Marjan Razavi, Hossein Hosseinzadeh
Saffron as a medicinal plant has many therapeutic effects. Phytochemical studies have reported that saffron is composed of at least four active ingredients which include crocin, crocetin, picrocrocin and safranal. The carotenoids of saffron are sensitive to oxygen, light, heat and enzymatic oxidization. However, regulation of these factors is required for saffron quality. Some pharmacologic effects of saffron and its active compounds include cardioprotective, neuroprotective, memory enhancer, antidepressant and anxiolytic...
November 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29119333/physiologically-based-pharmacokinetic-modelling-of-cytochrome-p450%C3%A2-2c9-related-tolbutamide-drug-interactions-with-sulfaphenazole-and-tasisulam
#12
Everett J Perkins, Maria Posada, P Kellie Turner, Jill Chappell, Wee Teck Ng, Chris Twelves
BACKGROUND AND OBJECTIVES: Cytochrome P450 2C9 (CYP2C9) is involved in the biotransformation of many commonly used drugs, and significant drug interactions have been reported for CYP2C9 substrates. Previously published physiologically based pharmacokinetic (PBPK) models of tolbutamide are based on an assumption that its metabolic clearance is exclusively through CYP2C9; however, many studies indicate that CYP2C9 metabolism is only responsible for 80-90% of the total clearance. Therefore, these models are not useful for predicting the magnitude of CYP2C9 drug-drug interactions (DDIs)...
November 8, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29116616/correction-to-continuous-infusion-versus-intermittent-bolus-of-beta-lactams-in-critically-ill-patients-with-respiratory-infections-a-systematic-review-and-meta-analysis
#13
Young R Lee, Pamela D Miller, Saeed K Alzghari, Delilah D Blanco, Jackson D Hager, Kailey S Kuntz
Unfortunately, ≥ was found missing between scores and 20 in conclusion section of the online published article. The original article was corrected.
November 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29101732/a-review-of-the-clinical-pharmacokinetics-and-pharmacodynamics-of-isavuconazole
#14
Kyle John Wilby
Invasive fungal infections are a major cause of morbidity and mortality, especially for immunocompromised patients. Treatment options are few and most are limited by safety and formulation concerns. Isavuconazole is a new triazole antifungal agent with official indications for the treatment of invasive fungal infections caused by Aspergillus and Mucormycosis. Its clinical efficacy has been proven in two landmark trials, SECURE and VITAL. This review aims to summarize and evaluate the published literature reporting clinical pharmacokinetic and pharmacodynamic outcome data of isavuconazole in humans...
November 4, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29076028/safety-tolerability-and-pharmacokinetics-of-oral-bi-425809-a-glycine-transporter-1-inhibitor-in-healthy-male-volunteers-a-partially-randomised-single-blind-placebo-controlled-first-in-human-study
#15
Viktoria Moschetti, Michael Desch, Sophia Goetz, Karl-Heinz Liesenfeld, Holger Rosenbrock, Klaus-Peter Kammerer, Glen Wunderlich, Sven Wind
BACKGROUND AND OBJECTIVES: Schizophrenia and Alzheimer's disease are characterised by glutamatergic pathway abnormalities related to N-methyl-D-aspartate (NMDA) receptor hypofunction and cognitive impairment. Glycine is an NMDA receptor co-agonist; inhibition of glycine transporter 1 (GlyT1) should improve NMDA receptor hypofunction. This study evaluated safety and pharmacokinetic properties of BI 425809-a potent and selective GlyT1 inhibitor. METHODS: In the single-rising dose (SRD) component of this study, subjects were randomised to a single dose of BI 425809 [doses (mg): 0...
October 26, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28890991/comments-on-population-pharmacokinetic-modeling-of-olmesartan-the-active-metabolite-of-olmesartan-medoxomil-in-patients-with-hypertension
#16
LETTER
Nuggehally R Srinivas
No abstract text is available yet for this article.
December 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28547295/high-loading-dose-of-microencapsulated-gliclazide-formulation-exerted-a-hypoglycaemic-effect-on-type-1-diabetic-rats-and-incorporation-of-a-primary-deconjugated-bile-acid-diminished-the-hypoglycaemic-antidiabetic-effect
#17
Svetlana Golocorbin-Kon, Jelena Calasan, Boris Milijasevic, Sasa Vukmirovic, Mladena Lalic-Popovic, Momir Mikov, Hani Al-Salami
BACKGROUND AND OBJECTIVE: Gliclazide is a drug commonly used in type 2 diabetes mellitus. Recently, gliclazide has shown desirable pharmacological effects such as immunoregulatory and anti-clotting effects, which suggests potential applications in type 1 diabetes mellitus (T1DM). Gliclazide has variable absorption after oral administration, and thus using targeted-delivery techniques, such as microencapsulation, may optimise gliclazide absorption and potential applications in T1DM. Bile acids such as cholic acid have shown microcapsule-stabilising and controlled-release effects, and thus their incorporation into gliclazide microcapsules may further optimise gliclazide release, absorption and antidiabetic effects...
December 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28536776/development-of-improved-dosing-regimens-for-mycophenolate-mofetil-based-on-population-pharmacokinetic-analyses-in-adults-with-lupus-nephritis
#18
Azrin N Abd Rahman, Susan E Tett, Halim A Abdul Gafor, Brett C McWhinney, Christine E Staatz
BACKGROUND AND OBJECTIVE: Mycophenolic acid (MPA) provides effective treatment for lupus nephritis patients. Owing to its large pharmacokinetic variability, it is questionable whether standard fixed dose therapy can achieve optimal MPA exposure. The aim of this study was to develop a population pharmacokinetic model of MPA and its metabolite, 7-O-MPA-β-glucuronide (MPAG), to identify important covariate influences and better predict patient dosing requirements. METHODS: MPA and MPAG concentration-time profiles were collected from 25 patients receiving mycophenolate mofetil (MMF) with or without cyclosporine (CsA) co-therapy...
December 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28536775/catechol-o-methyltransferase-and-udp-glucuronosyltransferases-in-the-metabolism-of-baicalein-in-different-species
#19
Ruiya Zhang, Yonglei Cui, Yan Wang, Xiangge Tian, Lu Zheng, HaiJian Cong, Bin Wu, Xiaokui Huo, Chao Wang, BaoJing Zhang, Xiaobo Wang, Zhonghui Yu
BACKGROUND: Baicalein is the major bioactive flavonoid in some herb medicines and dietary plants; however, the detailed metabolism pathway of its major metabolite oroxylin A-7-O-β-D-glucuronide in human was not clear. It was important to illustrate the major metabolic enzymes that participate in its elimination for the clinic use of baicalein. OBJECTIVES: We first revealed a two-step metabolism profile for baicalein and illustrated the combination of catechol-O-methyltransferase (COMT) and uridine diphosphate-glucuronosyltransferases (UGTs) in drug metabolism, further evaluated its bioactivity variation during drug metabolism...
December 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28536774/physiologically-based-pharmacokinetic-modelling-and-prediction-of-metformin-pharmacokinetics-in-renal-hepatic-impaired-young-adults-and-elderly-populations
#20
Su-Jin Rhee, Hyewon Chung, SoJeong Yi, Kyung-Sang Yu, Jae-Yong Chung
BACKGROUND AND OBJECTIVES: Physiologically based pharmacokinetic (PBPK) modelling and simulation enable researchers to overcome practical limitations for clinical trials on special populations. This study was conducted to investigate how the PBPK model describes the pharmacokinetics of metformin in young adult and elderly populations and to predict the pharmacokinetics of metformin in patients with renal or hepatic impairment in both populations. METHODS: A first-order absorption/PBPK model for metformin was built in the Simcyp simulator version 14 release 1...
December 2017: European Journal of Drug Metabolism and Pharmacokinetics
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